Substituted N-Phenylpyrazine-2-carboxamides: synthesis and antimycobacterial evaluation.
Molecules
; 14(10): 4180-9, 2009 Oct 20.
Article
in En
| MEDLINE
| ID: mdl-19924056
The condensation of chlorides of substituted pyrazinecarboxylic acids with ringsubstituted anilines yielded twelve substituted pyrazinecarboxylic acid amides. The synthetic approach, analytical, and lipophilicity data of the newly synthesized compounds are presented. Two antituberculosis assays were used. Firstly, the antimycobacterial activity against four different Mycobacterium strains in a series of pyrazine derivatives was investigated. Secondly, the antimycobacterial evaluation was performed at the Tuberculosis Antimicrobial Acquisition and Coordinating Facility (TAACF) program. Interesting in vitro antimycobacterial activity was found, N-(3-iodo-4-methylphenyl) pyrazine-2-carboxamide (9) was most active derivative compound against M. tuberculosis (MIC < 2.0 micromol/L), while another iodo derivative 5-tert-butyl-6-chloro-N-(3-iodo-4-methyl-phenyl)pyrazine-2-carboxamide (12) was the most active compound in the TAACF antituberculosis screening program (IC(90) = 0.819 microg/mL).
Full text:
1
Collection:
01-internacional
Database:
MEDLINE
Main subject:
Pyrazines
/
Mycobacterium kansasii
/
Mycobacterium avium
/
Mycobacterium tuberculosis
Language:
En
Journal:
Molecules
Journal subject:
BIOLOGIA
Year:
2009
Document type:
Article
Affiliation country:
Country of publication: